| GENERIC NAME: |
Estradiol Valerate
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| THERAPEUTIC CATEGORY: |
Sex Hormone
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| THERAPUETIC CLASS: |
Sex Hormone
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| PHARMACOLOGICAL CLASS: |
Estrogen ester
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| Composition: |
Each tablet contains: Estradiol valerate 1 mg
Each tablet contains: Estradiol valerate 2 mg
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| Pregnancy Category: |
X
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| Presentation: |
Available in the pack size as 10 tablets X 10 blisters
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| Mechanism of Action: |
Estradiol valerate is a synthetic, esterified prodrug of 17β-estradiol, acting as an estrogen receptor (ER) agonist to manage symptoms of menopause, hypogonadism, and various cancers. It works by binding to ERα and ERβ receptors in tissues like the uterus and brain, regulating Gene expression to mimic endogenous estrogen, thereby reducing gonadotropins (FSH/LH) and maintaining bone density.
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| Indications: |
- Hormone replacement therapy (HRT) for estrogen deficiency symptoms in peri- and postmenopausal women.
- Prevention of osteoporosis in postmenopausal women.
- Atropic Vaginitis.
- Hypogonadism.
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| Dosage: |
Route of administration: Oral
Children: Not applicable for this product
- Treatment to control menopausal symptoms should be initiated with Estradiol valerate 1 mg.
- If considered necessary, Estradiol valerate 2 mg should be used. Once treatment is established the lowest effective dose necessary for relief of symptoms should be used.
- For prevention of postmenopausal osteoporosis one tablet of Estradiol valerate 2 mg is to be taken daily.
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| Pharmacokinetics: |
Absorption: After oral intake, estradiol valerate is rapidly hydrolyzed in the intestine and liver to 17-estradiol and valeric acid.
Bioavailability: Oral bioavailability is low (~3%) due to extensive first-pass metabolism; most of the dose converts to metabolites such as estrone and estrone sulfate.
Peak Concentration: Maximum serum estradiol levels occur in 6–8 hours after a 2 mg tablet. Food may increase peak levels slightly but does not affect overall exposure.
Distribution: About 98% binds to plasma proteins (albumin ~61%, SHBG ~37%).
Elimination: Terminal half-life is 14–17 hours, with metabolites mainly excreted in urine.
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| Adverse Effects: |
- Breast pain
- Headache
- Vaginal itching or discharge
- Changes in menstrual period
- Thinning scalp hair
- Weight gain/loss
- Nausea and vomiting
- Bloating; stomach cramps
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| Contraindications: |
- Known hypersensitivity to Estradiol Valerate or any other components of the formulation
- Known, past or suspected breast cancer
- Estrogen-dependent malignant tumor
- Untreated endometrial hyperplasia
- Arterial or venous thromboembolism
- Liver disease
- Porphyria
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| WARNINGS AND PRECAUTIONS : |
- Caution is advised in patients with Leiomyoma (uterine fibroids) or endometriosis.
- Caution should be used in patients who suffers or previously suffered from diabetes mellitus with or without vascular involvement, hypertension, systemic lupus erythematous, epilepsy, asthma, otosclerosis or hereditary angiodema.
- During treatment, periodic check-ups are recommended of a frequency and nature adapted to the individual woman.
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